N-myristoyltransferase (NMT)

SC-58272 is a potent and selective inhibitor of N-myristoyltransferase (Nmt) in Candida albicans, exhibiting an IC50 of 56 nM against the strain B311. This compound demonstrates a 250-fold selectivity for the fungal enzyme when compared to the human counterpart. SC-58272 is valuable for research applications involving fungal pathogenesis and the study of myristoylation processes in C. albicans.

IMP-1088 is a highly potent dual inhibitor of human N-myristoyltransferases NMT1 and NMT2, exhibiting IC50 values of less than 1 nM for both isoforms and a Kd of under 210 pM for NMT1. This compound effectively inhibits rhinovirus replication by blocking the N-myristoylation of the virus-encoded protein VP0, thereby preventing the virus from completing its lifecycle. In addition, IMP-1088 offers protective effects to host cells by mitigating the cytotoxic consequences associated with viral infections, making it a valuable tool for research into antiviral therapies.

DDD85646 is a potent inhibitor of N-myristoyltransferase (NMT), specifically targeting the enzyme from Trypanosoma brucei with an IC50 of 2 nM and human NMT with an IC50 of 4 nM. This compound demonstrates significant potential for therapeutic applications in treating human African trypanosomiasis by disrupting lipid modifications essential for parasite survival. Its oral bioavailability further enhances its applicability in drug development for infectious diseases caused by trypanosomes.

3-Thiatetradecanoic acid is a fatty acid substrate for N-myristoyltransferase (NMT), playing a pivotal role in the metabolism of thiofatty acids. This compound is utilized in research studying lipid metabolism and protein modification processes, particularly in the context of membrane protein dynamics. Its unique properties enable investigations into the biological implications of thiofatty acids in various cellular environments.

DDD100097 is a potent inhibitor of the N-myristoyltransferase enzyme (TbNMT), exhibiting an IC50 value of 2 nM. This compound enhances blood-brain barrier permeability, making it a valuable tool in the investigation of therapeutic approaches for African trypanosomiasis. DDD100097 is suitable for research applications focused on the modulation of trypanosome biology and treatment strategies.

MYX1715 is a potent inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. This compound effectively inhibits the proliferation of LU0884 and LU2511 cell lines, demonstrating IC50 values of 44 nM and 9 nM, respectively. MYX1715 has shown significant antitumor activity against neuroblastoma and gastric cancer in murine models, and it may be exploited as an antibody-drug conjugate (ADC) toxin for targeted cancer therapies.

NMT-IN-3 is a selective inhibitor of N-myristoyltransferase (NMT) targeting Plasmodium vivax. With an IC50 of 38 mM, it demonstrates significant inhibitory activity against Pv NMT. This reagent is valuable for studying myristoylation processes in malaria research and evaluating potential therapeutic strategies against Plasmodium infections.

NMT-IN-1 is an inhibitor of Trypanosoma brucei N-myristoyltransferase (TbNMT) with an IC50 of 31 μM, demonstrating selectivity over human N-myristoyltransferase (hNMT) with an IC50 of 66 μM. This thiazolidinone compound acts by binding to the active site of TbNMT, effectively inhibiting the myristoyl transfer reaction catalyzed by the enzyme. NMT-IN-1 is valuable in research focused on developing anti-parasitic agents for human African trypanosomiasis (African sleeping sickness) and serves as a structural foundation for optimizing TbNMT inhibitors with improved efficacy and selectivity for therapeutic applications.

IMP-1002 is an inhibitor of N-myristoyltransferase (NMT) in Plasmodium species. By inhibiting myristoylation activity, IMP-1002 effectively blocks the development of the malaria parasite. This reagent is suitable for research applications aimed at understanding malaria pathology and exploring novel therapeutic strategies.

Myristoyl Coenzyme A Lithium is a specific inhibitor of N-myristoyltransferase (NMT), which plays a critical role in myristoylation, a process that is vital for viral proliferation and has increased activity in colon epithelial tumors compared to normal cells. This compound functions by blocking the demyristoylation process, thereby regulating NMT activity, which may contribute to its potential anticancer and antiviral properties. Myristoyl Coenzyme A Lithium is valuable for research applications focusing on cancer biology and viral infection mechanisms.

Zelenirstat is a potent dual inhibitor of N-myristoyltransferase (NMT), exhibiting IC50 values of 5 nM for NMT1 and 8 nM for NMT2. This orally active small molecule induces apoptosis in cancer cells and demonstrates anti-cancer activity by inhibiting early B cell receptor (BCR) signaling. Zelenirstat is a valuable tool for investigating the mechanisms underlying malignant lymphoma and other related malignancies.

LY134046 is an inhibitor of N-myristoyltransferase (NMT), primarily targeting norepinephrine N-methyltransferase in cardiovascular research. This compound produces sustained reductions in mean arterial blood pressure and heart rate without significantly altering norepinephrine concentrations in the rat brain. Notably, LY134046 does not engage with adrenergic or cholinergic receptors, indicating that its hypotensive and bradycardic effects operate independently of neurogenic tension. At a dosage of 40 mg/kg/day, LY134046 leads to significant inhibition of NMT activity in the hypothalamus and brainstem, thereby inducing central norepinephrine depletion.

NMT-IN-8 is a potent and selective inhibitor of N-myristoyl transferase (NMT), exhibiting an IC50 value of less than 10 nM. It effectively disrupts the catalyzed protein N-myristoylation by binding to the peptide binding pocket of NMT, thereby influencing critical biological pathways including protein trafficking, signal transduction, and viral replication. This compound is particularly relevant for research applications in oncology, such as MYC-addicted cancers and B-cell lymphoma, as well as in the study of infectious diseases, including malaria, HIV, and rhinovirus infections.